Department of Chemistry, Texas A&M University, Box 30012, College Station, TX, 77842, USA.
Department of Molecular & Cellular Medicine, Texas A&M University Health Science Center, College Station, TX, 77843, USA.
ChemMedChem. 2019 Sep 4;14(17):1575-1579. doi: 10.1002/cmdc.201900356. Epub 2019 Aug 7.
We hypothesized that conjugation of the near-infrared dye MHI-148 with the anti-leukemia drug dasatinib might produce a potential theranostic for glioblastoma. In fact, the conjugate was found to bind the kinases Src and Lyn, and to inhibit the viability of a glioblastoma cell line with significantly greater potency than dasatinib alone, MHI-148 alone, or a mixture of dasatinib and MHI-148 at the same concentration. It was also used to successfully image a subcutaneous glioblastoma tumor in vivo.
我们假设将近红外染料 MHI-148 与白血病药物达沙替尼缀合可能产生胶质母细胞瘤的潜在治疗诊断试剂。事实上，该缀合物被发现与激酶Src 和 Lyn 结合，并以比单独的达沙替尼、单独的 MHI-148 或相同浓度的达沙替尼和 MHI-148 混合物更显著的效力抑制胶质母细胞瘤细胞系的活力。它还成功地用于体内成像皮下胶质母细胞瘤肿瘤。
